bs-60088C

DATASHEET

Formulation powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 494.32

Formula: C22 H12 Br N3 O4 S

CAS Number: 1420071-30-2

InChi Key: ULBOWKXOFOTCMU-NLDKGBHCSA-N

InChi: InChI=1S/C22H12BrN3O4S/c23-12-2-4-13(5-3-12)26-21(29)18(31-22(26)24)10-14-6-8-17(30-14)11-1-7-15-16(9-11)20(28)25-19(15)27/h1-10,24H,(H,25,27,28)/b18-10-,24-22?

Smiles: N=C1S/C(=C\C2=CC=C(O2)C2C=C3C(=CC=2)C(=O)NC3=O)/C(=O)N1C1C=CC(Br)=CC=1

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

Bioymifi is a potent and selective small molecule agonist of DR5, identified by a high-throughput chemical screening for compounds that promote cell death in synergy with a small-molecule mimetic of Smac. Bioymifi directly targets DR5, specifically binds the ECD of DR5 (Kd ~1.2 μM), and induces the formation of DR5 aggregates and DR5 activation. Bioymifi induces caspase-8–dependent apoptosis, which occurs through a DR5-dependent extrinsic pathway but independent of TRAIL. Bioymifi is capable of acting as a single agent to induce DR5 clustering and aggregation, leading to apoptosis without the need for a Smac mimetic in a variety of cancer cell lines, even in U2OS and HT29 cell lines. Bioymifi could be a potential lead compound for the development of small-molecule TRAIL mimics targeting DR5 for cancer therapy.